Eckenfels A, Kruss B, Kuritsch W
Arzneimittelforschung. 1984;34(1):15-20.
Severe damage, even necrosis, has been noted in the past in man after accidental intra-arterial (i.a.) application of injectable preparations intended for intravenous (i.v.) or other parenteral administration. Various experimental models in animals have been developed to test an eventual i.a. incompatibility. Reasons are given for the methodology used by us in the central artery of the rabbit's ear with and without occlusion (harder and softer test variant). Herewith preparations of acetamidoeugenol and thiopental were tested to work out an appropriate measure. In comparison we investigated a series of "placebo solutions" with solvents or other excipients used in the formulation of injection solutions. The "placebos" investigated were then classified with regard to their i.a. compatibility, because in many cases an intra-arterial intolerance can be attributed to them as much as to the active principle. The choice of experimental animal model, the transferability of results to man as well as possible mechanisms taking place in an accidental i.a. application and in the development of ensuing damage are discussed.
过去已经注意到,人体在意外动脉内(i.a.)注射用于静脉内(i.v.)或其他胃肠外给药的注射制剂后会出现严重损伤,甚至坏死。已经开发了各种动物实验模型来测试最终的动脉内不相容性。给出了我们在兔耳中央动脉中使用的方法(有闭塞和无闭塞,即较硬和较软测试变体)的原因。据此测试了乙酰氨基丁香酚和硫喷妥钠制剂以制定适当的措施。相比之下,我们研究了一系列含有注射溶液配方中使用的溶剂或其他辅料的“安慰剂溶液”。然后根据它们的动脉内相容性对所研究的“安慰剂”进行分类,因为在许多情况下,动脉内不耐受与活性成分一样多地可归因于它们。讨论了实验动物模型的选择、结果向人类的可转移性以及在意外动脉内给药和随后损伤发展过程中可能发生的机制。